912356-09-3

Basic information

• Product Name: (3aR,12bS)-rel-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one
• Synonyms: (3aR,12bS)-rel-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one;Cis-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-Dibenz[2,3:6,7]oxepino[4,5-c]pyrrole-1-one;(3aR,12bS)-5-chloro-2-Methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-1-one
• CAS NO: 912356-09-3
• Molecular Formula: C17H14ClNO2
• Molecular Weight: 299.75156
• Mol File: 912356-09-3.mol
• Article Data: 7

Chemical Properties

• Appearance: /
• Density: 1.311
• Storage Temp.: 2-8°C
• Solubility: Dichloromethane; Methanol
• CAS DataBase Reference: (3aR,12bS)-rel-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one(CAS DataBase Reference)
• NIST Chemistry Reference: (3aR,12bS)-rel-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one(912356-09-3)
• EPA Substance Registry System: (3aR,12bS)-rel-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one(912356-09-3)

Safety Data

• Hazardous Substances Data: 912356-09-3(Hazardous Substances Data)

Usage

Uses

rel-(3aR,12bS)-5-Chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one is an intermediate in the synthesis of cis-Asenapine Maleate (A788045), which can be used in synthetic preparation of amines by activation of amides by chloromethylsilane and redn. with lithium aluminum hydride.

Upstream product

• 1035404-19-3 methyl-N-[2-(4-chloro-2-phenoxyphenyl)-1-oxo-ethyl]-N-methylglycinate 
• 1366179-34-1 tributylamine salt of 2-(2-(4-chlorophenoxy)phenyl)acetic acid 
• 912356-09-3 cis 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one 
• 934996-79-9 5-chloro-2-methyl-2,3-dihydro-1H-dibenzo[2,3:6,7]oxepino [4,5-c]pyrrole-1-one 
• 57486-68-7 methyl (2-chlorophenyl)acetate 
• 2444-36-2 2'-chloro-benzeneacetic acid 
• 1383781-81-4 3-[2-(4-chlorophenoxy)phenyl]-4-hydroxy-1-methylpyrrolidine-2-one 
• 1035404-18-2 [2-(4-chloro-phenoxy)-phenyl]-acetyl chloride 
• 57486-69-8 methyl 2-(2-bromophenyl)acetate 
• 1035404-17-1 ethyl N-[2-[2-(4-chlorophenoxy)phenyl]acetyl]-N-methylglycinate 
• 25563-04-6 o-(p-chlorophenoxy)phenylacetic acid 
• 106-48-9 4-chloro-phenol 
• 912356-09-3 cis-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one 
• 934996-80-2 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole-1-one 

Downstream Products

• 912356-09-3 trans-11-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one 
• 912356-09-3 trans 5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrol-1-one 
• 85650-55-1 asenapine maleate 
• 934996-80-2 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole-1-one 
• 912356-09-3 ((3aS,12bS)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrol-1-one) 
• 135883-16-8 (3aR,12bR)-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepin[4,5-c]pyrrole maleate 
• 1435938-33-2 asenapine maleate 

Relevant articles and documents

A process for the preparation of key intermediate asenapine

The invention provides a chemical synthesis method, in particular to a preparation method of a key intermediate [formula (III)] compound of asenapine capable of serving as a schizophrenia drug. In an anhydrous system, the intermediate [formula (III)] compound is obtained through dehydration of an intermediate [formula (II)] compound and anhydride under the action of a catalyst. The invention further provides a novel method for preparing asenapine by the intermediate [formula (III)]. The provided method has the advantages of simple operation, high yield, environment-friendliness, lower cost, stable technology and the like.

Processes for the preparation of 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole

This invention provides improved processes for the preparation of 5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenzo[2,3:6,7]oxepino[4,5-c]pyrrole, asenapine. These processes allow the preparation of asenapine at industrial scale in good yields and high stereoselectivity.

ASENAPINE MALEATE

Aspects of the present application relate to a microcrystalline monoclinic form of asenapine maleate represented by structural Formula (I); processes for its preparation; and pharmaceutically acceptable dosage forms thereof.